FRAX1036( FRAX1036 | FRAX-1036 | FRAX 1036 )

Catalog No. M17296 CAS No. 1432908-05-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

FRAX1036
Note

Research use only, not for human use.
Brief Description

FRAX-1036 is a effective and selective PAK1 inhibitor.
Description

FRAX1036 is a potent and selective PAK1 inhibitor. Administration of docetaxel with either FRAX1036, or PAK1 small interfering RNA oligonucleotides dramatically altered signaling to cytoskeletal-associated proteins, such as stathmin, and induced microtubule disorganization and cellular apoptosis. Live-cell imaging revealed that the duration of mitotic arrest mediated by docetaxel was significantly reduced in the presence of FRAX1036, and this was associated with increased kinetics of apoptosis.
In Vitro

FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively. FRAX1036 (2.5 μM) incombination with docetaxel alters stathmin phosphorylation, induces the apoptotic marker cleaved PARP and increases kinetics of apoptosis in MDA-MB-175 and HCC2911 cells; also alters microtubule organization, mitosis and cell fate in U2OS cells. Moreover, FRAX1036 shows significantly effective inhibition on U2OS cells. FRAX1036 (10 μM) affects the proliferation of non-small cell lung cancer (NSCLC) cells when added to KRAS prenylation inhibitors.
In Vivo

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Synonyms

FRAX1036 | FRAX-1036 | FRAX 1036
Pathway

Angiogenesis
Target

EGFR
Recptor

PAK1|PAK2|PAK4
Research Area

Cancer
Indication

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CAS Number

1432908-05-8
Formula Weight

518.05
Molecular Formula

C28H32ClN7O
Purity

>98% (HPLC)
Solubility

DMSO : 5.3 mg/mL. 10.23 mM;
SMILES

CCn1c2nc(ncc2cc(c1=O)c1c(cc(cc1)c1cncc(n1)C)Cl)NCCC1CCN(CC1)C
Chemical Name

6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one

1.Ong CC,etal.Breast Cancer Res. 2015 Apr 23;17:59.

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